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Cinnamic Acid Derivatives for Treating Metabolic Syndrome

Korea Health Industry Development Institute (KHIDI)South Korea

Abstract ID:

Cinnamic acid derivatives are good candidates to satisfy this unmet medical need

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Executive Summary

BioNutrigen, Inc (“BioNutrigen”) was organized in 1999 by scientists from the Korean Research Institute of Bioscience and Biotechnology. BioNutrigen has been focused on developing non-toxic natural products and materials from vegetables and fruits for prevention or treatment of adult disease such as obesity, diabetes and CV diseases.

Cinnamic acid derivatives were extracted from natural sources (e.g., apple, tea, potato, coffee, grape, plum and etc) and used to prevent and treat blood lipid level-related diseases such as hyperlipidemia, arteriosclerosis, angina pectoris, stroke and fatty liver. Use of novel cinnamic acid derivatives to treat or prevent Metabolic Syndrome are protected by worldwide patents held by BioNutrigen.

It estimates that there are nearly 86 million Metabolic Syndrome patients in the six major markets. There are no medicines approved for treatment for Metabolic Syndrome and the lack of a safe and effective medicine for this indication creates an unmet medical need in major global markets around the world.

Fig.1 Cinnamic acid derivatives

Cinnamic acid derivatives are good candidates to satisfy this unmet medical need. Promising preclinical data generated over the past 8 years by BioNutrigen scientists makes cinnamic acid derivatives a “first-in-class” series of compounds targeted at the Metabolic Syndrome indication. BioNutrigen is seeking co-development partners or licensing partners to fund the clinical development an innovative and promising medicine, cinnamic acid derivatives.

Key Technology Highlights

Lowering blood cholesterol level

Cinnamic acid derivatives can improve lipid metabolism and liver function. These drugs also inhibit plaque formation in the endothelium of the main artery and diminish formation of fatty liver, as shown below compared to other commercial agents.

Group

TC

(mg/dl)

TG

(mg/dl)

HDL-C

(mg/dl)

HDL/TC

(%)

GOT

(IU/l)

GPT

(IU/l)

Fatty streak (%)

A

Control

1995+ 472

170 +30

50 + 11

2.5 + 0.4

161+ 71

96 + 46

80 + 8

3.2 + 0.3

Lovastatin

1446 + 263

153 + 95

58 + 23

4.9 + 2.6

43 + 12

81 + 44

15 + 3

3.4 + 0.5

4-hydroxycinnamic acid

1517 + 417

167 + 43

57 + 28

3.7 + 1.3

59 + 45

74 + 49

24 + 11

2.7 + 0.3

3,4-dihydroxycinnamic acid

1559 + 347

139 + 46

53 + 13

3.4 + 0.4

99 + 49

40 + 27

13 + 5

2.6 + 0.3

3,4-dihydroxyhydrocinnamic acid

1256 + 150

108 + 22

80 + 23

6.3 + 1.6

55 + 20

90 + 83

16 + 1

2.6 + 0.3

Inhibition of HMG-CoA reductase activity

HMG-CoA reductase activities observed with the 4-hydroxycinnamic acid, 3,4-dihydroxycinnamic acid and 3,4-dihydroxyhydrocinnamic acid groups are lower than that of the Control group by 31 to 70%.